3,4-dichloro-1-(3-chlorophenyl)-1,5-dihydropyrrol-2-one | 501099-10-1

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡咯啉
• 英文名称: 3,4-dichloro-1-(3-chlorophenyl)-1,5-dihydropyrrol-2-one
• 英文别名: 2H-Pyrrol-2-one, 3,4-dichloro-1-(3-chlorophenyl)-1,5-dihydro-；3,4-dichloro-1-(3-chlorophenyl)-2H-pyrrol-5-one
• CAS: 501099-10-1
• 化学式: C₁₀H₆Cl₃NO
• 分子量: 262.523
• InChiKey: UFYUHVMPCFYOFV-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.2
• 重原子数：
  15
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.1
• 拓扑面积：
  20.3
• 氢给体数：
  0
• 氢受体数：
  1

反应信息

• 作为产物：
  描述：

  3-氯苯胺 在 三乙酰氧基硼氢化钠 作用下， 以 二氯甲烷 、 溶剂黄146 为溶剂， 反应 24.0h， 以65%的产率得到3,4-dichloro-1-(3-chlorophenyl)-1,5-dihydropyrrol-2-one
  参考文献：
  名称：

  Process for preparing highly functionalized gamma-butyrolactams and gamma-amino acids

  摘要：

  该发明涉及通过还原胺化法制备高度官能化的γ-丁内酰胺和γ-氨基酸，并公开了制备普拉巴林（一种具有理想药用活性的GABA类似物）的方法。

  公开号：

  US20030225149A1

文献信息

• One-pot reductive amination of aldehydes and ketones with α-picoline-borane in methanol, in water, and in neat conditions
  作者：Shinya Sato、Takeshi Sakamoto、Etsuko Miyazawa、Yasuo Kikugawa

  DOI：10.1016/j.tet.2004.06.045

  日期：2004.8

  A one-pot reductive amination of aldehydes and ketones with amines using alpha-picoline-borane as a reducing agent is described. The reaction has been carried out in Wolf, in H2O, and in neat conditions in the presence of small amounts of AcOH. This is a highly efficient and mild procedure that is applicable for a wide variety of substrates. In particular, this is the first successful demonstration that this type of reaction can be carried out in water and in neat conditions. (C) 2004 Elsevier Ltd. All rights reserved.
• First Direct Reductive Amination of Mucochloric Acid:  A Simple and Efficient Method for Preparing Highly Functionalized α,β-Unsaturated γ-Butyrolactams
  作者：Ji Zhang、Peter G. Blazecka、James G. Davidson

  DOI：10.1021/ol0274662

  日期：2003.2.1

  [GRAPHICS]The first direct reductive amination of mucochloric acid (1) has been accomplished. Reaction of 1 with various alkyl, aryl, and benzylamines, followed by reduction in the same pot, provides an efficient method of obtaining N-benzyl-3,4-dichloro-1,5-dihydro-pyrrol-2-one and N-aryl (or alkyl)-3,4-dichloro-1,5-dihydro-pyrrol-2-ones.
• Process for preparing highly functionalized gamma-butyrolactams and gamma-amino acids
  申请人：——

  公开号：US20030225149A1

  公开（公告）日：2003-12-04

  The invention relates to a process for preparing highly functionalized &ggr;-butyrolactams and &ggr;-amino acids by reductive amination of mucohalic acid or its derivatives, and discloses a process for preparing pregabalin, a GABA analog with desirable medicinal activity. 1

  该发明涉及通过还原胺化法制备高度官能化的γ-丁内酰胺和γ-氨基酸，并公开了制备普拉巴林（一种具有理想药用活性的GABA类似物）的方法。